Search results for "Biphenyl Compounds"

showing 10 items of 59 documents

Angiotensin Receptor Neprilysin Inhibition Compared With Enalapril on the Risk of Clinical Progression in Surviving Patients With Heart Failure

2015

Background— Clinical trials in heart failure have focused on the improvement in symptoms or decreases in the risk of death and other cardiovascular events. Little is known about the effect of drugs on the risk of clinical deterioration in surviving patients. Methods and Results— We compared the angiotensin-neprilysin inhibitor LCZ696 (400 mg daily) with the angiotensin-converting enzyme inhibitor enalapril (20 mg daily) in 8399 patients with heart failure and reduced ejection fraction in a double-blind trial. The analyses focused on prespecified measures of nonfatal clinical deterioration. In comparison with the enalapril group, fewer LCZ696-treated patients required intensification of med…

Angiotensin receptorVascular damage Radboud Institute for Health Sciences [Radboudumc 16]receptorsTetrazolesheart failureAngiotensin-Converting Enzyme InhibitorsKaplan-Meier EstimateSacubitrilAngiotensin; Heart failure; Neprilysin; Receptors; Aminobutyrates; Angiotensin Receptor Antagonists; Angiotensin-Converting Enzyme Inhibitors; Biomarkers; Double-Blind Method; Enalapril; Heart Failure; Humans; Kaplan-Meier Estimate; Natriuretic Peptide Brain; Neprilysin; Peptide Fragments; Risk Factors; Stroke Volume; Survivors; Tetrazoles; Treatment Outcome; Troponin; Disease Progression; Medicine (all); Cardiology and Cardiovascular Medicine; Physiology (medical)AngiotensinEnalaprilRisk FactorsEnalapril/therapeutic useNatriuretic Peptide BrainHeart Failure/bloodSurvivorsReceptorNeprilysinAminobutyrates: Systèmes cardiovasculaire & respiratoire [D03] [Sciences de la santé humaine]Troponin/bloodTroponinAngiotensin Receptor Antagonists/therapeutic useDrug CombinationsAngiotensin-Converting Enzyme Inhibitors/therapeutic useTreatment OutcomeTetrazoles/therapeutic useCardiologyDisease ProgressionValsartanNeprilysinHeart Failure/blood/drug therapy/physiopathologyCardiology and Cardiovascular Medicinemedicine.drugReceptormedicine.medical_specialtyHeart failureneprilysinAngiotensin Receptor Antagonistsreceptors angiotensinDouble-Blind MethodPhysiology (medical)Internal medicineRenin–angiotensin systemmedicineHumansheart failure neprilysin receptors angiotensinEnalaprilbusiness.industryBiphenyl CompoundsStroke Volumemedicine.diseasePeptide FragmentsEndocrinologyAminobutyrates/therapeutic useStroke Volume/physiologyHeart failureNatriuretic Peptide Brain/blood: Cardiovascular & respiratory systems [D03] [Human health sciences]businessNeprilysin/antagonists & inhibitorsPeptide Fragments/bloodSacubitril ValsartanBiomarkersBiomarkers/blood
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Synthesis and antioxidant evaluation of novel silybin analogues

2006

In this work, we evaluated the antioxidant properties of the eight novel silybin analogues for their capacity to scavenge free radicals including superoxide anion radicals and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals in vitro. Compound 7d demonstrated an excellent antioxidant effect in scavenging superoxide anion free radical with an IC50 value of 26.5 microM, while the IC50 of quercetin (the reference compound) was 38.1 microM. Compounds 7b, 7e, 7h showed certain scavenging activities for both types of free radicals.

AnionsAntioxidantDPPHRadicalmedicine.medical_treatmentDrug Evaluation PreclinicalMedicinal chemistryAntioxidantsInhibitory Concentration 50chemistry.chemical_compoundPicratesSuperoxidesDrug DiscoverymedicineOrganic chemistryIC50PharmacologyDose-Response Relationship DrugSuperoxideBiphenyl CompoundsAnion radicalsFree Radical ScavengersGeneral MedicineIn vitroHydrazinesModels ChemicalchemistrySpectrophotometrySilybinQuercetinQuercetinSilymarinJournal of Enzyme Inhibition and Medicinal Chemistry
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Identification of Biphenyl-Based Hybrid Molecules Able To Decrease the Intracellular Level of Bcl-2 Protein in Bcl-2 Overexpressing Leukemia Cells

2009

With the aim of enhancing the structural complexity and diversity of an existing collection of bi- and terphenyl compounds, we synthesized hybrid molecules comprising of spirocyclic ketones (a complexity-bearing core) and bi/terphenyls (privileged fragments). Compounds 1, 3, 4, and 6 showed well-defined activity on apoptosis and differentiation, making them potential leads for development as new anticancer agents and chemical probes to study signaling networks in neoplastic cells.

Antineoplastic AgentsApoptosisHL-60 CellsChemical synthesisStructure-Activity RelationshipLeukemia Myelogenous Chronic BCR-ABL PositiveTerphenyl CompoundsDrug DiscoverymedicineHumansSpiro CompoundsChemistryBiphenyl CompoundsCell DifferentiationBiological activityKetonesmedicine.diseaseIn vitroLeukemiaProto-Oncogene Proteins c-bcl-2BiochemistryApoptosisCell cultureMolecular MedicineTerphenyl CompoundsK562 CellsIntracellularJournal of Medicinal Chemistry
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The Antioxidant Potential of White Wines Relies on the Chemistry of Sulfur-Containing Compounds: An Optimized DPPH Assay

2019

The DPPH (2,2-Diphenyl-1-picrylhydrazyl) assay is an easy and efficient method commonly used to determine the antioxidant capacity of many food matrices and beverages. In contrast with red wines, white wines are poorer in antioxidant polyphenolics, and the more hydrophilic sulfur-containing compounds in them may contribute significantly to their antioxidant capacity. The modification of the classical DPPH method, with a methanol-buffer and the measure of EC20 (quantity of sample needed to decrease the initial DPPH concentration by 20%) has shown that sulfur-containing compounds such as cysteine (0.037 &plusmn

AntioxidantDPPHmedicine.medical_treatmentPharmaceutical ScienceMethanethiolWineantioxidant capacity01 natural sciencesAntioxidantsCatechinAnalytical ChemistryEC<sub>20</sub>Ferulic acidchemistry.chemical_compoundcaractérisation sensorielleDrug Discovery[SDV.IDA]Life Sciences [q-bio]/Food engineeringCaffeic acidFood sciencefood and beveragesCatechinChimical engineering04 agricultural and veterinary sciences040401 food science3. Good healthChemistryChemistry (miscellaneous)Alimentation et NutritionMolecular Medicinesulfur compoundscapacité antioxydanteCoumaric AcidsDPPH;antioxidant capacity;Chardonnay;white wine;EC20;sensory oxidation level;sulfur compoundswhite winesensory oxidation levelChardonnayArticlelcsh:QD241-4410404 agricultural biotechnologyCaffeic Acidslcsh:Organic chemistryPhenolsPicratesmedicineEC20Food and NutritionGénie chimiqueHumansPhysical and Theoretical ChemistryBiologyvin blanc010401 analytical chemistryOrganic ChemistryBiphenyl CompoundsGlutathione0104 chemical sciencesHigh-Throughput Screening AssayschemistryPolyphenolDPPHMolecules
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Antioxidant and neuroprotective effects of synthesized sintenin derivatives

2009

Three series of sintenin derivatives (compounds 1-14) were designed and prepared and their antioxidative and neuroprotective effects were evaluated. The in vitro models of scavenging 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals, chelating ferrous ions, inhibiting the rat brain homogenates lipid peroxidation, and protecting neurons damaged by hydrogen peroxide were employed for bioassays. It was found that sintenin derivatives 4 and 13 showed remarkable antioxidative and neuroprotective activities.

AntioxidantDPPHmedicine.medical_treatmentRadicalNeuroprotectionAntioxidantsRats Sprague-DawleyLipid peroxidationchemistry.chemical_compoundPicratesDrug DiscoverymedicineAnimalsChelationHydrogen peroxideCells CulturedChelating AgentsNeuronsPharmacologyChemistryBiphenyl CompoundsHydrogen PeroxideGeneral MedicineRatsBiphenyl compoundNeuroprotective AgentsBiochemistryLipid PeroxidationPropionatesJournal of Enzyme Inhibition and Medicinal Chemistry
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In Vitro Phytotoxicity and Antioxidant Activity of Selected Flavonoids

2012

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AntioxidantDPPHmedicine.medical_treatmentantioxidant activityMorinflavonoids; germination; radical elongation; antioxidant activity; structure/activityBiologyArticlestructure/activityAntioxidantsLepidium sativumCatalysisRaphanusInorganic Chemistrychemistry.chemical_compoundPicratesBotanymedicineheterocyclic compoundsFood sciencePhysical and Theoretical ChemistryMolecular BiologySpectroscopyFlavonoidsBiphenyl CompoundsfungiOrganic Chemistryfood and beveragesBiological activityCatechinGeneral MedicineComputer Science Applicationsradical elongationBiphenyl compoundgerminationchemistryflavonoidsQuercetinLuteolinInternational Journal of Molecular Sciences
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Succinobucol’s New Coat — Conjugation with Steroids to Alter Its Drug Effect and Bioavailability

2011

Synthesis, detailed structural characterization (X-ray, NMR, MS, IR, elemental analysis), and studies of toxicity, antioxidant activity and bioavailability of unique potent anti-atherosclerotic succinobucol-steroid conjugates are reported. The conjugates consist of, on one side, the therapeutically important drug succinobucol ([4-{2,6-di-tert-butyl-4-[(1-{[3-tert-butyl-4-hydroxy-5-(propan-2-yl)phenyl]sulfanyl}ethyl)sulfanyl]phenoxy}-4-oxo-butanoic acid]) possessing an antioxidant and anti-inflammatory activity, and on the other side, plant stanol/sterols (stigmastanol, β-sitosterol and stigmasterol) possessing an ability to lower the blood cholesterol level. A cholesterol-succinobucol prodr…

AntioxidantFree RadicalsStereochemistrymedicine.medical_treatmentStatic ElectricityAnti-Inflammatory AgentsBiological AvailabilityPharmaceutical ScienceprobucolArticleAntioxidantsAnalytical Chemistrylcsh:QD241-441Micechemistry.chemical_compoundPicrateslcsh:Organic chemistrySulfanylDrug DiscoverymedicineAnimalsHumansPhysical and Theoretical Chemistrysuccinobucol; phytosterol; atherosclerosis; cholesterol; probucolta317phytosterolStigmastanolClinical Trials as TopicMice Inbred BALB CMolecular StructurePhytosterolBiphenyl CompoundsOrganic Chemistrycholesterol3T3 CellsFibroblastsProdrugAscorbic acidBioavailabilityBiphenyl compoundchemistryChemistry (miscellaneous)Molecular MedicineSteroidsatherosclerosissuccinobucolMolecules; Volume 16; Issue 11; Pages: 9404-9420
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Polyphenol Characterization, Antioxidant and Skin Whitening Properties of Alnus cordata Stem Bark

2019

In this study, we investigated the phenolic composition of the crude extract (MeOH 80 %) of Alnus cordata (Loisel.) Duby stem bark (ACE) and its antioxidant and skin whitening properties. RP-LC-DAD analysis showed a high content of hydroxycinnamic acids (47.64 %), flavanones (26.74 %) and diarylheptanoids (17.69 %). Furthermore, ACE exhibited a dose-dependent antioxidant and free-radical scavenging activity, expressed as half-maximal inhibitory concentration (IC50 ): Oxygen radical absorbance capacity (ORAC, IC50 1.78 μg mL-1 )>Trolox equivalent antioxidant capacity (TEAC, IC50 3.47 μg mL-1 )>2,2-Diphenyl-1-picrylhydrazyl (DPPH, IC50 5.83 μg mL-1 )>β-carotene bleaching (IC50 11.58 μg mL-1 )…

AntioxidantOxygen radical absorbance capacityDPPHmedicine.medical_treatmentTrolox equivalent antioxidant capacityBioengineeringAlnus cordata; antimelanogenic activity; Betulaceae; mushroom tyrosinase; polyphenols; RP-LC-DAD analysis; zebrafish; Alnus; Animals; Antioxidants; Biphenyl Compounds; Enzyme Inhibitors; Monophenol Monooxygenase; Picrates; Plant Bark; Plant Extracts; Polyphenols; Skin; ZebrafishAlnus01 natural sciencesBiochemistryAntioxidantschemistry.chemical_compoundPicratesmedicineAnimalsFood scienceEnzyme InhibitorsMolecular BiologyIC50ZebrafishSkinbiologyMonophenol MonooxygenasePlant Extracts010405 organic chemistryBiphenyl CompoundsPolyphenolsSkin whiteningGeneral ChemistryGeneral Medicinebiology.organism_classificationAlnus cordata0104 chemical sciences010404 medicinal & biomolecular chemistrychemistryPolyphenolPlant BarkMolecular Medicine
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Anti-inflammatory activity of erycristagallin, a pterocarpene from Erythrina mildbraedii.

2003

Erycristagallin, a pterocarpene isolated from Erythrina mildbraedii, was tested in vitro for its antioxidant properties on the stable 2,2-diphenyl-1-pycryl-hydrazyl (DPPH) free radical and on the arachidonic acid metabolism. In addition, erycristagallin was tested on different experimental models of inflammation, such as the acute and chronic inflammation induced by the application of 12-O-tetradecanoylphorbol 13-acetate (TPA) on mice and the phospholipase A(2)-induced mouse paw oedema test. In the carrageenan-induced mouse paw oedema test, the ethyl acetate extract obtained from E. mildbraedii showed anti-inflammatory activity, and erycristagallin was isolated as the active principle. In v…

Antioxidantmedicine.drug_classDPPHmedicine.medical_treatmentAnti-Inflammatory AgentsInflammationPharmacologyCarrageenanHeterocyclic Compounds 4 or More RingsLeukotriene B4Anti-inflammatoryAntioxidantsPhospholipases Achemistry.chemical_compoundMicePicratesIn vivomedicineAnimalsEdemaRats WistarErythrinaPharmacologyPhospholipase AArachidonic AcidPlant ExtractsBiphenyl CompoundsEarFree Radical ScavengersIsoflavonesIn vitroHindlimbRatsBiphenyl compoundchemistryBiochemistryFemalemedicine.symptomEuropean journal of pharmacology
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Assessment of the anti-inflammatory activity and free radical scavenger activity of tiliroside

2003

Three flavonoids, gnaphaliin, pinocembrin and tiliroside, isolated from Helichrysum italicum, were studied in vitro for their antioxidant and/or scavenger properties and in vivo in different models of inflammation. In vitro tests included lipid peroxidation in rat liver microsomes, superoxide radical generation in the xanthine/xanthine oxidase system and the reduction of the stable radical 1,1-diphenyl-2-pycryl-hydrazyl (DPPH). Acute inflammation was induced by application of 12-O-tetradecanoylphorbol 13-acetate (TPA) to the mouse ear or by subcutaneous injection of phospholipase A(2) or serotonin in the mouse paw. Eczema provoked on the mouse ear by repeated administration of TPA was selec…

Antioxidantmedicine.drug_classmedicine.medical_treatmentAnti-Inflammatory AgentsIn Vitro TechniquesPharmacologyAnti-inflammatoryLipid peroxidationMicechemistry.chemical_compoundPicratesSuperoxidesIn vivoLeukocytesmedicineAnimalsHumansBenzopyransHypersensitivity DelayedRats WistarXanthine oxidasePeroxidaseFlavonoidsHelichrysumInflammationPharmacologySheepPinocembrinPlant ExtractsBiphenyl CompoundsFree Radical ScavengersFree radical scavengerRatsBiphenyl compoundHydrazineschemistryBiochemistryFlavanonesMicrosomes LiverFemaleLipid PeroxidationPhytotherapyEuropean Journal of Pharmacology
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